JNJ-67856633 是一种具有口服活性、第一类、有效、选择性和变构性 MALT1 protease 抑制剂。JNJ-67856633 在某些情况下导致肿瘤停滞。
货号:ajcx33082
CAS:2230273-76-2
分子式:C20H11F6N5O2
分子量：467.32
溶解度:DMSO : 125 mg/mL (267.48 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. JNJ-67856633 in some cases lead to tumor stasis[1][2][3].

JNJ-67856633 is effective and highly bioavailable in both mouse and rat tumors, and in some cases led to tumor stasis. JNJ-67856633 leads to potent in vivo pharmacodynamic shutdown in CD79b- as well as CARD11-mutant ABC-DLBCL models as measured by serum IL10 or uncleaved BCL10 levels in tumors[1][3].

Dose dependent inhibition of the generation of Tregs (CD4+CD25+FoxP3+) following CD3/28 stimulation was observed upon treatment with JNJ-67856633 suggesting a potential immune modulatory role of MALT1 inhibition[3].

[1]. Virtual meeting delivers first time drug structures
[2]. A Phase 1, First-in-Human, Open-Label Study of the Safety, Pharmacokinetics, and Pharmacodynamics of JNJ-67856633, an Inhibitor of MALT1, in Participants with NHL and CLL
[3]. Abstract 5690: Discovery of JNJ-67856633: A novel, first-in-class MALT1 protease inhibitor for the treatment of B cell lymphomas